| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
LG100268 selectively targets the retinoid X receptors (RXRs), which are nuclear receptors that form heterodimers with other nuclear receptors such as PPARs, LXR, and VDR. It binds to RXRα, RXRβ, and RXRγ with high affinity, with EC50 values of 4 nM, 3 nM, and 4 nM, respectively. By activating these receptors, LG100268 modulates the transcription of genes involved in a wide range of biological processes, including lipid metabolism, cell differentiation, and inflammation. Its selectivity for RXRs over RARs makes it a specific tool for studying RXR-mediated pathways without the confounding effects of RAR activation.
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| ln Vitro |
In RAW264.7 cells, LG100268 (100 nM-1 μM; 24 hours) caused a 2.5-fold reduction in CXCL2 and IL-1β mRNA expression, as well as downregulation of CSF3 [3].
In vitro, LG100268 potently activates RXRα, RXRβ, and RXRγ with EC50 values of 4 nM, 3 nM, and 4 nM, respectively. It induces transcriptional activation in adipocytes. It affects the expression of various genes, including inhibiting keratin 17 expression in black lip epithelial cells and increasing PD-L1 expression in HER2 or triple-negative breast cancer cells. These in vitro activities confirm its potent and selective RXR agonist activity and its ability to modulate gene expression. |
| ln Vivo |
More than either C/P or LG268 alone, LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) and C/P together decreased mean tumor burden. In comparison to the control group, the combination significantly decreased lung tumors by 82% (as opposed to 59%–67% with the single drug) [3].
In vivo, LG100268 is orally active. It has been shown to influence RXRs and their partner receptors, such as Foxl2/Dmrt1, to induce masculinization in juvenile flatfish. This demonstrates its ability to exert biological effects in a living organism. Its activity in regulating gene expression and differentiation makes it a valuable tool for studying the physiological and pathological roles of RXR signaling in vivo. |
| Enzyme Assay |
Non-cell-based assays for LG100268 typically involve receptor binding and activation studies. In a cell-free system, the compound's ability to bind to RXR can be measured using techniques such as fluorescence polarization or surface plasmon resonance. The purified RXR ligand-binding domain is incubated with a fluorescently labeled RXR ligand and varying concentrations of LG100268. The compound's ability to displace the labeled ligand is measured, and its binding affinity (IC50 or Ki) is determined.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: RAW264.7 Cell Tested Concentrations: 100 nM-1 μM Incubation Duration: 24 hrs (hours) Experimental Results: LPS-induced decrease in cytokine mRNA levels. In vitro cellular assays for LG100268 are performed using cells that express RXR. A common assay is the reporter gene assay, where cells are transfected with a plasmid containing a luciferase gene under the control of an RXR response element. The cells are treated with LG100268 at various concentrations, and luciferase activity is measured. The increase in luciferase activity is directly proportional to RXR activation, allowing for the determination of an EC50 value. These assays provide a quantitative measure of the compound's agonist activity. |
| Animal Protocol |
Animal/Disease Models: A/J mice [3]
Doses: 50 mg/kg (in combination with carboplatin (50 mg/kg ip) starting 1 week after LG268 treatment diet) Route of Administration: Oral diet; one time/day; 7 weeks Experimental Results: Lung tumor growth in mice was Dramatically diminished. In vivo animal models for LG100268 would typically involve the use of rodents or other model organisms. The compound is administered orally, and its effects on RXR target gene expression and physiological parameters are assessed. For example, in studies of adipocyte differentiation, animals could be treated with LG100268, and the expression of adipocyte-specific genes in adipose tissue could be measured. These studies are crucial for understanding the in vivo pharmacology of the compound. |
| ADME/Pharmacokinetics |
LG100268 has a molecular formula of C23H25NO2 and a molecular weight of 347.45 g/mol. It is orally active, indicating good bioavailability. The compound is soluble in DMSO. Detailed PK parameters such as half-life and volume of distribution are not extensively detailed in the provided search results. It is typically stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for LG100268 are not provided in the search results. As a potent RXR agonist, its toxicity profile would be a key consideration. Given the role of RXRs in various physiological processes, potential side effects could be broad. The compound is intended for research use only and is not for human consumption.
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| References |
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| Additional Infomation |
LG-100268 is a retinoic acid X receptor (RXR) selective compound.
LG100268 is a potent, selective, and orally active retinoid X receptor (RXR) agonist. It has EC50 values of 4 nM for RXRα and RXRγ, and 3 nM for RXRβ. It displays >1000-fold selectivity for RXR over RAR. It activates RXR homodimers to induce transcriptional activation. It is used as a research tool for studying RXR-mediated signaling and has the CAS number 153559-76-3. |
| Molecular Formula |
C24H29NO2
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|---|---|
| Molecular Weight |
363.5
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| Exact Mass |
363.22
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| CAS # |
153559-76-3
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| PubChem CID |
3922
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| Appearance |
White to off-white solid powder
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| Density |
1.115g/cm3
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| Boiling Point |
487ºC at 760mmHg
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| Melting Point |
275-277ºC
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| Flash Point |
248.3ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
5.517
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SLXTWXQUEZSSTJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H29NO2/c1-15-12-18-19(23(4,5)9-8-22(18,2)3)13-17(15)24(10-11-24)20-7-6-16(14-25-20)21(26)27/h6-7,12-14H,8-11H2,1-5H3,(H,26,27)
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| Chemical Name |
6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid
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| Synonyms |
LG-100268.; LG 100268 ; LG100268
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5.56 mg/mL (~15.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.56 mg/mL (1.54 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.56 mg/mL (1.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7510 mL | 13.7552 mL | 27.5103 mL | |
| 5 mM | 0.5502 mL | 2.7510 mL | 5.5021 mL | |
| 10 mM | 0.2751 mL | 1.3755 mL | 2.7510 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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